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J B Fernandes

Publications and source records attributed to J B Fernandes.

17 recordsLinked to original sources
PubMed2005

Screening of Leishmania APRT enzyme inhibitors.

Adenine phosphoribosyltransferase (APRT) enzyme from Leishmania tarentolae has been proposed as a target for the rational search of new leishmanicidal drugs. In this paper, we describe the evaluation of the inhibitory activity on L. tarentolae APRT enzyme of 46 crude extracts of Meliaceae and Rutaceae plants, besides three furoquinolone alkaloids. The results showed that 21 extracts were able to decrease the APRT enzymatic activity (IA% > or = 50). The methanolic extracts from roots and leaves of Cedrela fissilis and from fruits, branches and leaves of Cipadessa fruticosa have showed strong activities. Therefore, these species could be a promising source of lead compounds for the rational design of new leishmanicidal drugs. The phytochemical investigation of an active fraction from Almeidea rubra afforded the alkaloids isodutaduprine, isoskimmianine and isokokusagine, which showed low to moderate activity on APRT.

Adenine Phosphoribosyltransferase↗
PubMed2004

In vivo tissue characterization using magnetic techniques.

Among the few non-invasive methods to quantify liver iron deposits, magnetic resonance imaging (MRI) and biomagnetic liver susceptometry (BLS) have been considered the best to evaluate iron overload in the body. This diagnosis is necessary for patients who regularly receive red blood cells transfusion and that have a genetic disorder known as hemochromatosis. In this work, we present the evaluation of the clinical usefulness of MRI and BLS of hepatic tissue to quantify iron deposits in non-transfused and transfused patients. Liver iron evaluation by MRI and BLS were performed in a group of 48 patients. The MRI images weighted in T2 were acquired using multi-slice single-spin-echo (SSE) and single-slice multi-spin-echo (MSE), conducted on a 1.5 T whole body scanner. BLS measurements were performed using an ac superconducting susceptometer based on SQUID. Typically MRI is able to evaluate iron overload in liver as high as 30 mg/g(dry tissue) when using MRI scanners provided with specially designed pulse sequences. For higher iron concentrations susceptibility measurement works better than MRI to evaluate higher iron overloads in the liver, because in this case there is saturation of MRI signal.

Adolescent↗
PubMed2004

Behavioral changes in workers of the leaf-cutting ant Atta sexdens rubropilosa induced by chemical components of Eucalyptus maculata leaves.

The response of Atta sexdens rubropilosa Forel workers to essential oils, epicuticular wax and hexane, dichloromethane, ethyl acetate, and methanol extracts of Eucalyptus maculata was evaluated. Hexane extracts of E. maculata interfered with the recognition mechanism among workers. The main active compounds identified from this plant were the sesquiterpenes elemol and beta-eudesmol. These compounds may be responsible for the resistance of this species to ant attack.

Animals↗
PubMed2002

Structure of Trypanosoma cruzi glycosomal glyceraldehyde-3-phosphate dehydrogenase complexed with chalepin, a natural product inhibitor, at 1.95 A resolution.

The structure of the glycosomal glyceraldehyde-3-phosphate dehydrogenase (gGAPDH) from Trypanosoma cruzi complexed with chalepin, a natural product from Pilocarpus spicatus, has been determined by X-ray crystallography to 1.95 A resolution. The structure is in the apo form without cofactors in the subunits of the tetrameric gGAPDH in the asymmetric unit. Unequivocal density corresponding to the inhibitor was clearly identified in one monomer. The final refined model of the complex shows extensive conformational changes when compared with the native structure. The mode of binding of chalepin to gGAPDH and its implications for inhibitor design are discussed.

Animals↗
PubMed2001

Toxicity of synthetic piperonyl compounds to leaf-cutting ants and their symbiotic fungus.

The development of Leucoagaricus gongylophorus, the fungus cultured by the leaf-cutting ant Atta sexdens was inhibited in vitro by synthetic compounds containing the piperonyl group. In addition, worker ants that were fed daily on an artificial diet to which these compounds were added had a higher mortality rate than the controls. The inhibition of the fungal growth increased with the size of the carbon side chain ranging from C1 through C8 and decreasing thereafter. 1-(3,4-Methylenedioxybenzyloxy)octane (compound 5) was the most active compound and inhibited the fungal development by 80% at a concentration of 15 micrograms ml-1. With worker ants the toxic effects started with compound 5 and increased with the number of carbons in the side chain. Thus, for the same concentration (100 micrograms ml-1) the mortality rates observed after 8 days of diet ingestion were 82%, 66% and 42%, for 1-(3,4-methylenedioxybenzyloxy)decane, 1-(3,4-methylenedioxybenzyloxy)dodecane and compound 5, respectively, whereas with commercial piperonyl butoxide the mortality was 68%. The latter compound, which is known as a synergist insecticide, was as inhibitory to the symbiotic fungus as the synthetic compound 5. The possibility of controlling these insects in the future using compounds that can target simultaneously both organisms is discussed.

Animals↗
PubMed2001

Sesquiterpene pyridine alkaloids from Peritassa campestris.

An investigation of the methanol and ethyl acetate extracts from the roots of Peritassa campestris (Hippocrateaceae) afforded the sesquiterpene pyridine alkaloid, 4-hydroxy-7-epi-chuchuhuanine E-V, and nine known alkaloids, forrestine, euonimine, ebenifoline E-I, wilforine, euojaponine F, euonine, wilforjine, neowilforine, and wilforzine. The structures of the isolates were elucidated on the basis of spectral data, particularly HMQC and HMBC experiments.

Alkaloids↗
PubMed2001

Chemistry and bioactivity of Raulinoa echinata Cowan, an endemic Brazilian Rutaceae species.

The hexane extract of the stems of Raulinoa echinata afforded the sesquiterpenes germacrene D (6), 1beta,6alpha-dihydroxy-4-(15)-eudesmene (4) and oplopanone (5); the triterpenes squalene, isomultiflorenol (7), isobauerenol (8) and friedelin (9); the protolimonoids melianone (2) and melianodiol (3); and the pyranocoumarin 3-(1'-1'-dimethylallyl)-lomatin (1), which has not been reported previously as a natural product; together with beta-sitosterol. The hexane extract and some of these compounds were assayed in vitro against trypomastigote forms of Trypanosoma cruzi. Brine shrimp lethality and antimicrobial activities of the crude extract and pure compounds were also evaluated.

Animals↗
PubMed2000

Pyrano chalcones and a flavone from Neoraputia magnifica and their Trypanosoma cruzi glycosomal glyceraldehyde-3-phosphate dehydrogenase-inhibitory activities.

The fruits of Neoraptua magnifica var. magnifica afforded three new flavonoids: 2'-hydroxy-4,4',-dimethoxy-5',6'-(2'',2''-dimethylpyrano)chalcone, 2'-hydroxy-3,4,4'-trimethoxy-5',6'-(2'',2''-dimethylpyrano)chalcone, and 3',4'-methylenedioxy-5,7-dimethoxyflavone which were identified on the basis of spectroscopic methods. The known flavonoids 2'-hydroxy-3,4,4',5-tetramethoxy-5',6'-(2'',2''-dimethylpyrano)chalcone, 2'-hydroxy-3,4,4',5,6'-pentamethoxychalcone, 3',4'-methylenedioxy-5,6,7-trimethoxyflavone, 3',4'-methylenedioxy-5',5,6,7-tetramethoxyflavone, 3',4',5',5,7-pentamethoxyflavanone and 3',4',5'5,7-pentamethoxyflavone were also identified. The latter flavone was the most active as glyceraldehyde-3-phosphate dehydrogenase-inhibitor.

Animals↗
PubMed2000

A limonoid from Trichilia estipulata.

The limonoid 21,24,25,26,27-pentanor-15,22-oxo-7alpha,23-dihydroxy-apotirucalla(eupha)-1-en-3-one was isolated from the dichloromethane extract of the stem bark of Trichilia estipulata. Its structure was established by spectroscopic methods (UV, EIMS, 1H and 13C NMR, HMQC and HMBC).

Limonins↗
PubMed2000

Anthrone and oxanthrone C,O-diglycosides from Picramnia teapensis.

Two C,O-diglycosylated compounds, the anthrone picramnioside F, and the oxanthrone mayoside C, were isolated from the stem bark of Picramnia teapensis, along with the previously reported anthraquinones, 1-O-beta-D- and 8-O-beta-D-glucopyranosyl emodin. The compounds were separated by recycling-HPLC, and their structures were determined on the basis of spectroscopic analysis. CD measurements were used to establish the absolute configuration of the anthrone and oxanthrone. The antifungal activity of 1-O-beta-D- and 8-O-beta-D-glucopyranosyl emodin against Leucoagaricus gongilophorus was shown to be similar to that of the lignan sesamin.

Chromatography, High Pressure Liquid↗
PubMed2000

In vitro activity of Rutaceae species against the trypomastigote form of Trypanosoma cruzi.

The activity of crude plant extracts of nine species of Rutaceae against the trypomastigote form of Trypanosoma cruzi was evaluated at 4 mg/ml. Thirty-two crude extracts were tested and eight of them showed significant activity (>80%). The most active extract was obtained from the stems of Pilocarpus spicatus (97.3%). Fractionation of the active crude extracts provided 25 fractions which were tested against the trypomastigote form of T. cruzi at 2 mg/ml. Of these six showed significant activity (>80%). The most active fractions (100%) were obtained from the leaves of Almeidea coerulea (butanol fraction) and Conchocarpus inopinatus (dichloromethane fraction).

Animals↗
PubMed1998

New polyketides from the sponge Plakortis sp.

Fractionation of the MeOH extract of the sponge Plakortis sp. collected around the Amirantes Islands yielded four novel polyketides (4-7). The structures have been established by a detailed highfield 2D NMR study.

Animals↗
PubMed1993

Comparative investigation of the effects of the immunosuppressants cyclosporine A, cyclosporine G, and FK-506 on platelet activation.

We have determined that ADP-induced platelet aggregation and secretion are enhanced by preincubation of human platelets with the immunosuppressant cyclosporine A (CSA) (see accompanying article by Naik et al., 1993). In the present report we compare the effects of CSA with two other potent immunosuppressants, cyclosporine G (CSG), an analogue of CSA, and FK-506, on platelet activation. Preincubation of platelets with either CSA, CSG, or FK-506 resulted in platelets which exhibited hyperaggregability when stimulated by ADP. CSG produced the lowest degree of hyperaggregation, whereas FK-506 produced the highest at an equivalent concentration. All three compounds enhanced the secretion of serotonin, with FK-506 producing the highest degree of serotonin release and CSG producing the lowest amount. Platelet hyperaggregation and enhanced secretion were both time- and dose-dependent. Comparative studies performed with CSA and CSG indicated that a short preincubation period with CSA (2.5 min) resulted in a 90% enhancement of ADP-induced platelet aggregation, whereas CSG enhancement was only 20%. At a concentration of 600 ng/ml, CSA produced 120% enhancement of ADP-induced platelet aggregation, whereas CSG produced only a 30% enhancement. Several potential mechanisms responsible for the enhanced ADP-induced aggregation and secretion were investigated. Determination of the binding of two radiolabeled probes directed against the fibrinogen receptor, fibrinogen itself, and a monoclonal antibody (M.Ab.G10) revealed that the binding of fibrinogen to ADP-stimulated platelets was enhanced by 50% following the preincubation of platelets with 600 ng/ml CSA. Smaller, yet significant enhancement occurred in the presence of CSG. Similar results were obtained when M.Ab.G10 was used. Preincubation of platelets with 600 ng/ml CSA or CSG resulted in 60% and 30% increase in total protein kinase C activity, respectively, following the addition of ADP. In conclusion, this study has determined that preincubation of platelets with CSA or FK-506 (CSG, to a smaller extent) results in significant enhancement of ADP-induced platelet aggregation and secretion. The hyperaggregation and hypersecretion observed may be due to an enhanced expression of fibrinogen receptors on the platelet surface resulting from an increase in protein kinase C activity.

Antibodies, Monoclonal↗
PubMedDate not supplied

Separation and NMR studies on lignans of Raulinoa echinata.

Investigation of the leaves of Raulinoa echinata Cowan (Rutaceae) has led to the isolation of several furofuran (2,6-diaryl-3,7-dioxabicyclo[3.3.0]-octane) lignan derivatives, namely (+)-sesamin, (+)-eudesmin, (+)-methylpiperitol (= kobusin), (+)-piperitol-gamma,gamma-dimethylallylether and the corresponding epi compounds: (+)-asarinin, (+)-epieudesmin, (+)-methylxanthoxylol, (+)-methylpluviatilol, (+)-xanthoxylol-gamma,gamma-dimethylallylether and (+)-pluviatilol-gamma,gamma-dimethylallylether. This is the first report of the chromatographic separation of the epimers (+)-methylxanthoxylol/(+)-methylpluviatilol and (+)-xanthoxylol-gamma,gamma-dimethylallylether/(+)-pluviatilol-gamma,gamma- dimethylallylether and of their NMR nOe difference studies.

Dioxoles↗
PubMedDate not supplied

Studies towards the detection and identification of sesquiterpene pyridine alkaloids in Peritassa campestris by mass spectrometry.

Sesquiterpene pyridine alkaloids were analysed in Peritassa campestris by mass spectrometric techniques such as ESI-MSMS and GCMS. Ten alkaloids previously isolated from this plant and fully identified by other physical methods, including NMR spectroscopy and X-ray diffraction, were carefully studied by MS. It was observed that the low mass ions detected at m/z 178 and 206 in both MS technique tested were characteristic of evoninic and wilfordic acids, which are part of the macrolactone in these sesquiterpene alkaloids. The intensity of a fragment ion detected at m/z 93 in CAD, and especially in EI, spectra was found to be diagnostic in distinguishing between evoninoates and wilfordates. Running parent/daughter or GCMS experiments enabled these substances to be detected in crude fractions of P. campestris. Parent ion scans of m/z 206 were very as a first analysis of an alkaloid mixture.

Alkaloids↗
PubMedDate not supplied

Limonoids from the endemic Brazilian species Raulinoa echinata.

Phytochemical survey of stems and leaves of the South Brazilian endemic Raulinoa echinata Cowan, Rutaceae led to the isolation of five limonoid derivatives: the widespread limonin, limonexic acid, kihadalactone B, a methoxylated limonexic acid derivative and a degraded limonoid structurally related to fraxinellone. The two latter compounds have been isolated for the first time. These compounds displayed weak inhibitory activity when assayed in vitro against trypomastigote forms of Trypanosoma cruzi. In this paper, the isolation, structure elucidation and bioactivity of these compounds are reported.

Animals↗